Process for the Preparation of Cathin

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent describes a method for producing cathine ((1S, 2S)-norpseudoephedrine), a compound with stimulant effects, using a two-step, enzyme-catalyzed process. In the first step, benzaldehyde is converted with an acetyl donor by an (S)-selective lyase, and in the second step, the resulting intermediate is transformed using an (S)-selective transaminase with an amine donor to yield highly enantiomerically pure cathine. The process can use enzymes in purified form or in genetically engineered microorganisms, and it requires few steps and is scalable.

Use CasesContent extracted from patent full text and abstract with AI.

• Industrial manufacture of cathine for pharmaceutical applications, such as appetite suppressants or cardiovascular stimulants.
• Biocatalytic production of chiral amines for fine chemical or active pharmaceutical ingredient (API) synthesis.
• Academic or industrial research into enzymatic or biotechnological routes for the production of complex organic compounds.
• Production of cathine as a reference standard in analytical laboratories.

BenefitsContent extracted from patent full text and abstract with AI.

• Enables a simple, cost-effective synthesis of cathine with high purity (>99% enantiomeric excess, high diastereomeric purity).
• Reduces the number of synthesis steps compared to traditional chemical processes, improving overall yield and process efficiency.
• Uses commercially available and potentially renewable starting materials.
• Requires fewer purification and work-up steps, facilitating easy scale-up to industrial levels.
• Allows use of enzymes in both isolated or whole-cell (in vivo) formats, increasing flexibility and potential for biotechnological optimization.
• Minimizes unwanted by-products by using selective enzymes, resulting in a cleaner process.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention relates to a process for producing cathine ((1S, 2S)-norpseudoephedrine), in which, in a first reaction step, benzaldehyde is reacted with an acetyl donor of formula (1), where R = H or COOH, using an (S)-selective lyase, to yield an enantiomer mixture according to formulas (2) and (3) and, in a second step, the compound according to formula (3) is reacted with an amine donor using an (s)-selective transaminase to yield (1S, 2S)-norpseudoephedrine.